Search

Your search keyword '"Rob Kania"' showing total 2 results
Start Over Author "Rob Kania"
2 results on '"Rob Kania"'

1. Preclinical characterization of an intravenous coronavirus 3CL protease inhibitor for the potential treatment of COVID19

Author

Britton Boras, Rhys M. Jones, Brandon J. Anson, Dan Arenson, Lisa Aschenbrenner, Malina A. Bakowski, Nathan Beutler, Joseph Binder, Emily Chen, Heather Eng, Holly Hammond, Jennifer Hammond, Robert E. Haupt, Robert Hoffman, Eugene P. Kadar, Rob Kania, Emi Kimoto, Melanie G. Kirkpatrick, Lorraine Lanyon, Emma K. Lendy, Jonathan R. Lillis, James Logue, Suman A. Luthra, Chunlong Ma, Stephen W. Mason, Marisa E. McGrath, Stephen Noell, R. Scott Obach, Matthew N. O’ Brien, Rebecca O’Connor, Kevin Ogilvie, Dafydd Owen, Martin Pettersson, Matthew R. Reese, Thomas F. Rogers, Romel Rosales, Michelle I. Rossulek, Jean G. Sathish, Norimitsu Shirai, Claire Steppan, Martyn Ticehurst, Lawrence W. Updyke, Stuart Weston, Yuao Zhu, Kris M. White, Adolfo García-Sastre, Jun Wang, Arnab K. Chatterjee, Andrew D. Mesecar, Matthew B. Frieman, Annaliesa S. Anderson, and Charlotte Allerton

Subjects
Science
Abstract

The 3CL protease of SARS-CoV-2 is inhibited by PF-00835231 in vitro. Here, the authors show that the prodrug PF-07304814 has broad spectrum activity, inhibiting SARS-CoV and SARS-CoV-2 in mice and its ADME and safety profile support clinical development.

Published
2021
Full Text
View/download PDF

2. Preclinical characterization of an intravenous coronavirus 3CL protease inhibitor for the potential treatment of COVID19

Author

Heather Eng, Annaliesa S. Anderson, Norimitsu Shirai, Brandon J. Anson, James Logue, Stuart Weston, Marisa McGrath, Martyn D. Ticehurst, Rebecca E. O’Connor, Michelle Rossulek, Martin Pettersson, Matthew N O' Brien, Jean G. Sathish, Matthew B. Frieman, Emi Kimoto, Jun Wang, R. Scott Obach, Emily I. Chen, Robert Haupt, Yuao Zhu, Thomas F. Rogers, Andrew D. Mesecar, Suman Luthra, Adolfo García-Sastre, Dafydd R. Owen, Rhys M. Jones, Eugene P. Kadar, Chunlong Ma, Rob Kania, Lisa Aschenbrenner, Arnab K. Chatterjee, Charlotte Moira Norfor Allerton, Joseph John Binder, Kevin Ogilvie, Holly L. Hammond, Nathan Beutler, Claire M. Steppan, Jennifer Hammond, Stephen Noell, Romel Rosales, Robert M. Hoffman, Lillis Jonathan Richard, Matthew R. Reese, Stephen W. Mason, Dan Arenson, Malina A. Bakowski, Lawrence W. Updyke, Lorraine F. Lanyon, Kris M. White, Emma K. Lendy, Melanie G. Kirkpatrick, and Britton Boras

Subjects
Indoles, Science, medicine.medical_treatment, viruses, General Physics and Astronomy, Pharmacology, medicine.disease_cause, General Biochemistry, Genetics and Molecular Biology, Virus, Article, Mice, In vivo, Coronavirus 229E, Human, Leucine, Chlorocebus aethiops, medicine, Animals, Humans, Protease inhibitor (pharmacology), skin and connective tissue diseases, Infusions, Intravenous, Vero Cells, Coronavirus 3C Proteases, Coronavirus, ADME, Multidisciplinary, Protease, Alanine, Chemistry, SARS-CoV-2, fungi, COVID-19, Drug Synergism, General Chemistry, Prodrug, In vitro, Adenosine Monophosphate, Pyrrolidinones, respiratory tract diseases, COVID-19 Drug Treatment, body regions, Disease Models, Animal, Coronavirus Protease Inhibitors, Severe acute respiratory syndrome-related coronavirus, Drug Design, Drug Therapy, Combination, HeLa Cells
Abstract

COVID-19 caused by the SARS-CoV-2 virus has become a global pandemic. 3CL protease is a virally encoded protein that is essential across a broad spectrum of coronaviruses with no close human analogs. PF-00835231, a 3CL protease inhibitor, has exhibited potent in vitro antiviral activity against SARS-CoV-2 as a single agent. Here we report, the design and characterization of a phosphate prodrug PF-07304814 to enable the delivery and projected sustained systemic exposure in human of PF-00835231 to inhibit coronavirus family 3CL protease activity with selectivity over human host protease targets. Furthermore, we show that PF-00835231 has additive/synergistic activity in combination with remdesivir. We present the ADME, safety, in vitro, and in vivo antiviral activity data that supports the clinical evaluation of PF-07304814 as a potential COVID-19 treatment.

Published
2021

Catalog

Books, media, physical & digital resources
See catalog results